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Assay Detail

CHEMBL4150584

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of JAK2 (unknown origin) using FAM-labeled peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 25 mins in presence of ATP
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Janus Kinase 2 (JAK2) and Histone Deacetylase (HDAC) Dual Inhibitors as a Novel Strategy for the Combinational Treatment of Leukemia and Invasive Fungal Infections.
Huang Y, Dong G, Li H, Liu N, Zhang W, Sheng C.
J Med Chem (2018) 61 : 6056 -6074
PubMed 29940115 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168763 1 9.00
CHEMBL4175964 1 9.00
CHEMBL4172110 1 9.00
CHEMBL4159366 1 8.70
CHEMBL4167286 1 8.70
CHEMBL4164238 1 8.70
CHEMBL4167685 1 8.70
CHEMBL4160833 1 8.52
CHEMBL4162254 1 8.40
CHEMBL4175555 1 8.10
CHEMBL4170168 1 8.10
CHEMBL4169802 1 7.82
CHEMBL4168707 1 7.80
CHEMBL4165344 1 7.75
CHEMBL1078178 MOMELOTINIB 4.0 1 7.39
CHEMBL4160840 1 7.07
CHEMBL4168767 1 6.96
CHEMBL98 VORINOSTAT 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168763 IC50 = 1.0 nM 9.00
CHEMBL4175964 IC50 = 1.0 nM 9.00
CHEMBL4172110 IC50 = 1.0 nM 9.00
CHEMBL4159366 IC50 = 2.0 nM 8.70
CHEMBL4167286 IC50 = 2.0 nM 8.70
CHEMBL4164238 IC50 = 2.0 nM 8.70
CHEMBL4167685 IC50 = 2.0 nM 8.70
CHEMBL4160833 IC50 = 3.0 nM 8.52
CHEMBL4162254 IC50 = 4.0 nM 8.40
CHEMBL4175555 IC50 = 8.0 nM 8.10
CHEMBL4170168 IC50 = 8.0 nM 8.10
CHEMBL4169802 IC50 = 15.0 nM 7.82
CHEMBL4168707 IC50 = 16.0 nM 7.80
CHEMBL4165344 IC50 = 18.0 nM 7.75
CHEMBL1078178 MOMELOTINIB IC50 = 41.0 nM 7.39
CHEMBL4160840 IC50 = 85.0 nM 7.07
CHEMBL4168767 IC50 = 110.0 nM 6.96
CHEMBL98 VORINOSTAT IC50 - -